For research use only. Not for therapeutic Use.
RN486 (Cat.No:I000963) is a small molecule inhibitor that targets Bruton’s tyrosine kinase (BTK). It has shown efficacy in preclinical studies for the treatment of B-cell malignancies, such as B-cell lymphomas and chronic lymphocytic leukemia (CLL). RN486’s selective inhibition of BTK signaling pathways offers potential as a targeted therapy in hematological malignancies.
| Catalog Number | I000963 |
| CAS Number | 1242156-23-5 |
| Synonyms | 6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one |
| Molecular Formula | C₃₅H₃₅FN₆O₃ |
| Purity | ≥95% |
| Target | Btk |
| Solubility | DMSO: ≤ 24 mg/mL |
| Storage | Store at -20℃ |
| IC50 | 4.0 nM [1] |
| IUPAC Name | 6-cyclopropyl-8-fluoro-2-[2-(hydroxymethyl)-3-[1-methyl-5-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]-6-oxopyridin-3-yl]phenyl]isoquinolin-1-one |
| InChI | InChI=1S/C35H35FN6O3/c1-39-12-14-41(15-13-39)26-8-9-32(37-19-26)38-30-18-25(20-40(2)34(30)44)27-4-3-5-31(28(27)21-43)42-11-10-23-16-24(22-6-7-22)17-29(36)33(23)35(42)45/h3-5,8-11,16-20,22,43H,6-7,12-15,21H2,1-2H3,(H,37,38) |
| InChIKey | ZTUJNJAKTLHBEX-UHFFFAOYSA-N |
| SMILES | CN1CCN(CC1)C2=CN=C(C=C2)NC3=CC(=CN(C3=O)C)C4=C(C(=CC=C4)N5C=CC6=CC(=CC(=C6C5=O)F)C7CC7)CO |
| Reference | </br>1:Structure-based drug design of RN486, a potent and selective Bruton/’s tyrosine kinase (BTK) inhibitor, for the treatment of rheumatoid arthritis. Lou Y, Han X, Kuglstatter A, Kondru RK, Sweeney ZK, Soth M, McIntosh J, Litman R, Suh J, Kocer B, Davis D, Park J, Frauchiger S, Dewdney N, Zecic H, Taygerly JP, Sarma K, Hong J, Hill RJ, Gabriel T, Goldstein DM, Owens TD.J Med Chem. 2015 Jan 8;58(1):512-6. doi: 10.1021/jm500305p. Epub 2014 Apr 16. PMID: 24712864 </br>2:Suppression of glomerulonephritis in lupus-prone NZB × NZW mice by RN486, a selective inhibitor of Bruton/’s tyrosine kinase. Mina-Osorio P, LaStant J, Keirstead N, Whittard T, Ayala J, Stefanova S, Garrido R, Dimaano N, Hilton H, Giron M, Lau KY, Hang J, Postelnek J, Kim Y, Min S, Patel A, Woods J, Ramanujam M, DeMartino J, Narula S, Xu D.Arthritis Rheum. 2013 Sep;65(9):2380-91. doi: 10.1002/art.38047. PMID: 23754328 Free Article</br>3:RN486, a selective Bruton/’s tyrosine kinase inhibitor, abrogates immune hypersensitivity responses and arthritis in rodents. Xu D, Kim Y, Postelnek J, Vu MD, Hu DQ, Liao C, Bradshaw M, Hsu J, Zhang J, Pashine A, Srinivasan D, Woods J, Levin A, O/’Mahony A, Owens TD, Lou Y, Hill RJ, Narula S, DeMartino J, Fine JS.J Pharmacol Exp Ther. 2012 Apr;341(1):90-103. doi: 10.1124/jpet.111.187740. Epub 2012 Jan 6. PMID: 22228807 Free Article |
